SCD inhibitor | CAS:1032229-33-6

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のSCD inhibitor(CAS:1032229-33-6)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:A939572; stearoyl-CoA desaturase (SCD) inhibitor; SCD-inhibitor
Cat. No. :CS-0305
CAS No. :1032229-33-6
Formula:C20H22ClN3O3
M. Wt. : 387.86
Solubility:DMSO: ≥ 56 mg/mL

A939572 is a potent, and orally bioavailable SCD1 inhibitor with IC50 values of mSCD1 and hSCD1, respectively.IC50 & Target: IC50: [1]In Vitro: A939572 exhibits robust in vivo activity with dose-dependent desaturation index lowering effects[1].A939572 is a small molecule that specifically inhibits SCD1 enzymatic activity. A939572 demonstrates a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC50s of 65 nM, 50 nM, 65 nM, and 6 nM, respectively). In A939572 (SCDi) treated Caki1 and A498 cells, all five ER stress related genes are expressed at significantly increased levels compared to DMSO+BSA control, and this elevated expression can be blocked with the addition of OA-BSA[2]. In Vivo: Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts are treated with A939572 (30mg/kg, p.o.) and Tem individually or in combination over the course of four weeks, and tumor volume (mm3) is recorded. A939572 and Tem monotherapy generate similar growth responses with approximately 20-30% reductions in tumor volume (vs. placebo control) being observed upon study completion, with values reaching statistical significance only within the last week of treatment. The combination group yields over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment[2].

von Roemeling CA, et al. Stearoyl-CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Clin Cancer Res. 2013 May 1;19(9):2368-80. Xin Z, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302.